GNE-7915 - LRRK2 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGNE-7915Cat. No.: HY-18163CAS No.: 1351761-44-8分式: CHFNO分量: 443.4作靶点: LRRK2作通路: Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 14.33 mg/mL (32.32 mM; Need ultrasonic and warming)M

2、ass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2553 mL 11.2765 mL 22.5530 mL5 mM 0.4511 mL 2.2553 mL 4.5106 mL10 mM 0.2255 mL 1.1277 mL 2.2553 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 GNE-7915效选择性，可渗透脑的LRRK2抑制剂，IC50值为9 nM。IC50 & Target IC50: 9 nM 1 (LRRK2)体外研究Maintai

3、ning the methoxy/fluoro arrangement at C-2/C-5 and varying aminoalkyl R1 substitution resultes insingle-digit nanomolar LRRK2 cellular activities for GNE-7915 and compound 19. Expanded Invitrogenkinase profiling (187 kinases) at 0.1 M for both GNE-7915 (100-fold over LRRK2 Ki) and 19 (250-fold over1

4、/2 Master of Small Molecules 您边的抑制剂师www.MedChemELRRK2 Ki) resultes in only TTK showing greater than 50% inhibition. Selectivity profiling using the DiscoverXKinomeScan55 competitive binding assay panel, which includes 392 unique kinases, is also performed forGNE-7915 at 0.1 M. Binding of 50% probe d

5、isplacement is detected for 10 kinases and of 65% for onlyLRRK2, TTK, and ALK, further supporting the excellent LRRK2 selectivity for GNE-7915. Cerep receptorprofiling, including expanded brain panels, suggestes that GNE-7915 and 19 only inhibite 5-HT2B with 70%inhibition at 10 M. GNE-7915 and 19 ar

6、e confirmed to be moderately potent 5-HT2B antagonists in vitrofunctional assays 2.户使本产品发表的科研献 Hum Mol Genet. 2017 Jul 15;26(14):2747-2767. Programa Oficial de Doctorado en Biomedicina. Universidad de Granada. 5-Jul-2017. Harvard Medical School LINCS LIBRARYSee more customer validations on HYPERLINK

7、 / www.MedChemEREFERENCES1. Kavanagh ME, et al. The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg Med ChemLett. 2013 Jul 1;23(13):3690-6.2. Estrada AA, et al. Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small moleculeinhibitors. J Med Chem. 2012 Nov 26;55(22):9416-33.McePdfHeightCaution: Product has not been fully validated for medical applications.For researc